MA26946A1 - NEW PYRAZOLE DERIVATIVES AND THEIR USE AS PROTEIN-KINASE INHIBITORS. - Google Patents
NEW PYRAZOLE DERIVATIVES AND THEIR USE AS PROTEIN-KINASE INHIBITORS.Info
- Publication number
- MA26946A1 MA26946A1 MA27050A MA27050A MA26946A1 MA 26946 A1 MA26946 A1 MA 26946A1 MA 27050 A MA27050 A MA 27050A MA 27050 A MA27050 A MA 27050A MA 26946 A1 MA26946 A1 MA 26946A1
- Authority
- MA
- Morocco
- Prior art keywords
- formula
- compounds
- syndrome
- kinase inhibitors
- pyrazole derivatives
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/38—Nitrogen atoms
- C07D231/40—Acylated on said nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Reproductive Health (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Neurosurgery (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Gynecology & Obstetrics (AREA)
- Psychiatry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pregnancy & Childbirth (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
DEPOSANT Société dite : PFIZER PRODUCTS INC. REVENDICATION DE PRIORITES US 31 Aoét 2000 60/229,415 Voir en annexe le titre de l'invention et le texte de l'abrégé Dérivés de pyrazole nouveaux et leur utilisation comme inhibiteurs de protéine-kinases L'invention propose des composés de formule (1) dans laquelle R1, R2, R3 et R4 répondent aux définitions, et leurs sels pharmaceutiquement acceptables. Les composés de formule (1) sont indiqués en tant qu'agents ayant une activité inhibitrice de cdk2, et GSK-3. Des compositions pharmaceutiques et méthodes comprenant des composés de formule (1) pour le traitement et la prévention de maladies et d'affections comprenant une croissance cellulaire anormale, telle qu'un cancer, et des maladies et affections neuro-dégénératives ainsi que celles affectées par la neurotransmission de la dopamine. Il est décrit également des compositions et méthodes pharmaceutiques, comprenant des composés de formule (1) pour le traitement de la stérilité masculine et de la motilité du sperme ; du diabète sucré ; d'une tolérance entravée au glucose ; du syndrome métabolique ou syndrome X ; du syndrome d'ovaire polykystique ; de 1'adipogénèse et de l'obésité ; de la myogénèse et de la fragilité, par exemple du déclin des performances physiques dé à l'??ge ; de la sarcopénie aigue, par exemple de l'atrophie musculaire et/ou de la cachexie associées aux brélures, à l'état alité, à une immobilisation des membres ou à une intervention chirurgicale thoracique, abdominale et/ou orthopédique importante ; de la septicémie ; de la perte des cheveux, de l'éclaircissement capillaire et de la calvitie ; et d'une immunodéficience.DEPOSITOR Company known as: PFIZER PRODUCTS INC. CLAIM OF PRIORITIES US 31 August 2000 60 / 229,415 See appendix the title of the invention and the text of the abstract New pyrazole derivatives and their use as protein kinase inhibitors The invention provides compounds of formula (1) wherein R1, R2, R3 and R4 meet the definitions, and their pharmaceutically acceptable salts. The compounds of formula (1) are indicated as agents having an inhibitory activity of cdk2, and GSK-3. Pharmaceutical compositions and methods comprising compounds of formula (1) for the treatment and prevention of diseases and conditions including abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions as well as those affected by the neurotransmission of dopamine. Pharmaceutical compositions and methods are also described, comprising compounds of formula (1) for the treatment of male sterility and sperm motility; diabetes mellitus; impaired glucose tolerance; metabolic syndrome or syndrome X; polycystic ovary syndrome; adipogenesis and obesity; myogenesis and frailty, for example the decline in physical performance from age; acute sarcopenia, for example muscle atrophy and / or cachexia associated with burns, in bed state, immobilization of the limbs or major thoracic, abdominal and / or orthopedic surgery; sepsis; hair loss, hair thinning and baldness; and immunodeficiency.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22941500P | 2000-08-31 | 2000-08-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MA26946A1 true MA26946A1 (en) | 2004-12-20 |
Family
ID=22861151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA27050A MA26946A1 (en) | 2000-08-31 | 2003-02-21 | NEW PYRAZOLE DERIVATIVES AND THEIR USE AS PROTEIN-KINASE INHIBITORS. |
Country Status (38)
| Country | Link |
|---|---|
| EP (1) | EP1313710A1 (en) |
| JP (1) | JP2004507526A (en) |
| KR (1) | KR20030027093A (en) |
| CN (1) | CN1518543A (en) |
| AP (1) | AP2001002266A0 (en) |
| AR (1) | AR035345A1 (en) |
| AU (1) | AU2001280009A1 (en) |
| BG (1) | BG107455A (en) |
| BR (1) | BR0113574A (en) |
| CA (1) | CA2420363A1 (en) |
| CR (1) | CR6881A (en) |
| CZ (1) | CZ2003468A3 (en) |
| DO (1) | DOP2001000243A (en) |
| DZ (1) | DZ3398A1 (en) |
| EA (1) | EA200300205A1 (en) |
| EC (1) | ECSP034480A (en) |
| EE (1) | EE200300085A (en) |
| GT (1) | GT200100179A (en) |
| HN (1) | HN2001000192A (en) |
| HR (1) | HRP20030140A2 (en) |
| HU (1) | HUP0302669A3 (en) |
| IL (1) | IL154016A0 (en) |
| IS (1) | IS6687A (en) |
| MA (1) | MA26946A1 (en) |
| MX (1) | MXPA03001785A (en) |
| NO (1) | NO20030958L (en) |
| NZ (1) | NZ523656A (en) |
| OA (1) | OA12368A (en) |
| PA (1) | PA8528101A1 (en) |
| PE (1) | PE20020470A1 (en) |
| PL (1) | PL360742A1 (en) |
| SK (1) | SK2002003A3 (en) |
| SV (1) | SV2002000618A (en) |
| TN (1) | TNSN01132A1 (en) |
| UY (1) | UY26909A1 (en) |
| WO (1) | WO2002018346A1 (en) |
| YU (1) | YU14703A (en) |
| ZA (1) | ZA200301064B (en) |
Families Citing this family (85)
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|---|---|---|---|---|
| ATE538794T1 (en) | 1999-01-13 | 2012-01-15 | Bayer Healthcare Llc | GAMMA CARBOXYARYL SUBSTITUTED DIPHENYL UREA COMPOUNDS AS P38 KINASE INHIBITORS |
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| RU2319693C9 (en) | 1999-01-13 | 2008-08-20 | Байер Копэрейшн | Derivatives of urea (variants), pharmaceutical composition (variants) and method for treatment of diseases associated with cancer cells growth (variants) |
| US7473691B2 (en) | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6610677B2 (en) | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6613776B2 (en) | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ATE346064T1 (en) | 2000-09-15 | 2006-12-15 | Vertex Pharma | PYRAZOLE COMPOUNDS AS PROTEIN KINASE INHIBITORS |
| WO2002068415A1 (en) | 2000-12-21 | 2002-09-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ES2289143T3 (en) * | 2001-09-27 | 2008-02-01 | Laboratoires Serono Sa | METHODS TO INCREASE THE LEVELS OF ENDOGENA TESTOSTERONE. |
| SI1478358T1 (en) | 2002-02-11 | 2013-09-30 | Bayer Healthcare Llc | Sorafenib tosylate for the treatment of diseases characterized by abnormal angiogenesis |
| US20030216396A1 (en) | 2002-02-11 | 2003-11-20 | Bayer Corporation | Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
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| JP4733388B2 (en) | 2002-08-02 | 2011-07-27 | バーテックス ファーマシューティカルズ インコーポレイテッド | Pyrazole compositions useful as inhibitors of GSK-3 |
| JP2006504725A (en) | 2002-10-09 | 2006-02-09 | ファイザー・プロダクツ・インク | Pyrazole compounds for the treatment of neurodegenerative disorders |
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| JP2006519234A (en) * | 2003-02-27 | 2006-08-24 | スミスクライン ビーチャム コーポレーション | New compounds |
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| GB0317127D0 (en) * | 2003-07-22 | 2003-08-27 | Astex Technology Ltd | Pharmaceutical compounds |
| EP1663978B1 (en) | 2003-07-23 | 2007-11-28 | Bayer Pharmaceuticals Corporation | Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions |
| JP2006528661A (en) * | 2003-07-25 | 2006-12-21 | ファイザー・インク | Aminopyrazole compounds and use as CHK1 inhibitors |
| DK1689721T3 (en) * | 2003-11-26 | 2010-09-20 | Pfizer Prod Inc | Aminopyrazole derivatives as GSK-3 inhibitors |
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| DK1047418T3 (en) * | 1997-12-22 | 2005-11-21 | Bayer Pharmaceuticals Corp | Inhibition of raf kinase by substituted heterocyclic ureas |
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2001
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